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Posted by Bennie Sue ( on February 08, 2000 at 18:12:26:

In Reply to: GABAPENTIN ??? posted by Bob on February 08, 2000 at 16:40:02:

Bet you found this already. Anyway, this is what Alta Vista produced. It's for seizures primarily, they say.

Neurontin (gabapentin capsules) is supplied as imprinted hard shell capsules containing 100 mg, 300 mg, and 400 mg of gabapentin. The inactive ingredients are lactose, corn starch, and talc. The 100-mg capsule shell contains gelatin and titanium dioxide. The 300-mg capsule shell contains gelatin, titanium oxide, and yellow iron oxide. The 400-mg capsule shell contains gelatin, red iron oxide, titanium dioxide, and yellow iron oxide. The imprinting ink contains FD&C Blue No. 2 and titanium dioxide.

Gabapentin is described as 1-(aminomethyl)cyclohexanacetic acid with an empirical formula of C9H17NO2 and a molecular weight of 171.24.

Gabapentin is a white to off-white crystalline solid. It is freely soluble in water and both basic and acidic aqueous solutions.

Clinical Pharmacology:
Mechanism of Action
The mechanism by which gabapentin exerts its anticonvulsant action is unknown, but in animal test systems designed to detect anticonvulsant activity, gabapentin prevents seizures as do other marketed anticonvulsants. Gabapentin exhibits anti-seizure activity in mice and rats in both the maximal electroshock and pentylenetetrazol seizure models and other preclinical models (e.g., strains with genetic epilepsy, etc.). The relevance of these models to human epilepsy is not known.

Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid) but it does not interact with GABA receptors, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. Gabapentin was tested in radioligand binding assays at concentrations up to 100 mcM and did not exhibit affinity for a number of other common receptor sites, including benzodiazepine, glutamate, N-methyl-D-aspartate (NMDA), quisqualate, kainate, strychnine-insensitive or strychnine-sensitive glycine, alpha 1, alpha 2, or beta adrenergic, adenosine A1 or A2, cholinergic muscarinic or nicotinic, dopamine D1 or D2, histamine H1, serotonin S1 or S2, opiate mu, delta or kappa, voltage-sensitive calcium channel sites labeled with nitrendipine or diltiazem, or at voltage-sensitive sodium channel sites with batrachotoxinin A 20-alpha-benzoate.

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